Assay Detail
Functional
CHEMBL744039
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist potency against carbachol induced contractions of isolated guinea pig ileum Muscarinic acetylcholine receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Muscarinic acetylcholine receptor M3 (CHEMBL5498) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Structure-activity relationships among methoctramine-related polymethylene tetraamines. Chain-length and substituent effects on M-2 muscarinic receptor blocking activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 6 | 6.43 | 8.83 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL517712 | ATROPINE | 4.0 | 1 | 8.83 |
| CHEMBL114885 | — | — | 1 | 6.38 |
| CHEMBL170793 | — | — | 1 | 6.15 |
| CHEMBL169523 | — | — | 1 | 5.48 |
| CHEMBL169290 | — | — | 1 | 5.31 |
| CHEMBL168235 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL517712 | ATROPINE | Kd | = | 1.479 | nM | 8.83 |
| CHEMBL114885 | — | Kd | = | 416.87 | nM | 6.38 |
| CHEMBL170793 | — | Kd | = | 707.95 | nM | 6.15 |
| CHEMBL169523 | — | Kd | = | 3311.31 | nM | 5.48 |
| CHEMBL169290 | — | Kd | = | 4897.79 | nM | 5.31 |
| CHEMBL168235 | — | Kd | > | 10000.0 | nM | - |